Neeraj Agrawal, A Rohini, M J N Chandrasekar, I J Singhvi, J Dwivedi , P C Sharma, K Gupta , N Brar
||Inventi Impact Med Chem, 2011, Vol.2011
Diclofenac, a non-steroidal anti-inflammatory drug suffers from the side effects of upper GI damage (stomach and duodenum) including lesions ulcers and life threatening perforations and hemorrhage along with short biological half-life. A polymeric prodrug of diclofenac has been synthesized in the present work to overcome the limitations associated with the drug. The diclofenac was coupled to chloro derivative of hydroxy propyl methacrylate (HPMA) to get polymerisable monomeric drug conjugate which was in turn subjected to radicular polymerization to get the polymeric prodrug. The synthesized prodrug was characterized by IR, NMR and Mass spectroscopy. The prodrug was evaluated for its drug content and subjected for in vitro drug release studies in buffer solutions of pH 1.2 and 7.4... mimicking the pH of upper and lower gastro intestinal tract. The drug release studies of the prodrug revealed its potential to release the drug predominantly at lower GI tract and in a sustained manner resulting in reduced GI disturbances and increased biological half life of the drug.